产品说明书

BT2

Print
Chemical Structure| 34576-94-8 同义名 : -
CAS号 : 34576-94-8
货号 : A760956
分子式 : C9H4Cl2O2S
纯度 : 97%
分子量 : 247.098
MDL号 : MFCD00781745
存储条件：

粉末 Sealed in dry,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(242.82 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 Impaired branched-chain amino acids (BCAA) catabolism plays a pivotal role in the pathogenesis of metabolic and neurological diseases. The mitochondrial branched-chain α-ketoacid dehydrogenase complex (BCKDC) kinase (BDK) inhibitors that augment BCKDC flux have been shown to reduce BCAA concentrations in vivo. BT2 is a novel BDK inhibitor with an IC50 value of 3.19 μM. In wild-type MEF cells, BT2 robustly stimulated BCKDC activity at concentration of 40 μM for 48 h. Administration of BT2 at 20 mg/kg/day to wild-type mice for 1 week led to nearly complete dephosphorylation and maximal activation of BCKDC in heart, muscle, kidneys, and liver with reduction in plasma BCAA concentrations[3].
作用机制 Mechanism: BT2 binds to an allosteric site in the N-terminal domain of each monomer in homodimeric BDK[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

4.05mL

0.81mL

0.40mL

20.23mL

4.05mL

2.02mL

40.47mL

8.09mL

4.05mL
参考文献

[1]Tso SC, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.

[2]Friberg A, et al. Discovery of potent myeloid cell leukemia 1 (Mcl-1) inhibitors using fragment-based methods and structure-based design. J Med Chem. 2013 Jan 10;56(1):15-30.

[3]Tso SC, Gui WJ, Wu CY, et al. Benzothiophene carboxylate derivatives as novel allosteric inhibitors of branched-chain α-ketoacid dehydrogenase kinase. J Biol Chem. 2014 Jul 25;289(30):20583-93.